西罗莫司脂化物|T2145

Temsirolimus
162635-04-3

￥313 2mg 起订

￥472 5mg 起订

￥738 10mg 起订

上海更新日期：2024-12-02

TargetMol中国（陶术生物）

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联系人：邵小姐

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产品详情:

中文名称：: 西罗莫司脂化物

英文名称：: Temsirolimus

CAS号：: 162635-04-3

品牌：: TargetMol

产地：: 美国

保存条件：: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

纯度规格：: 99.64%

产品类别：: 抑制剂

货号：: T2145

Product Introduction

Bioactivity

名称	Temsirolimus
描述	Temsirolimus (CCI-779) is a specific mTOR inhibitor ( IC50: 1.76 μM), used in the treatment of advanced renal cell cancer.
细胞实验	For all experiments, cells were plated in six-well plates in complete growth media for overnight. Various doses of CCI-779 or rapamycin analogs were added alone or with FK506 for indicated periods of time. Total cellular lysates were prepared using NuPAGE-LDS sample buffer. Equal amounts of proteins were subjected to immunoblotting analysis using NuPAGE electrophoresis system. Immunoblots were probed with appropriate primary and secondary antibodies following the manufacturer's instructions and detected using enhanced chemiluminescence. β-Actin immunoblotting and/or reversible Ponceau-S staining of nitrocellulose membranes after the transfer was used to visualize the total protein loading [1].
激酶实验	The Flag-tagged wild-type human mTOR (Flag-mTOR) and Flag-mTOR-SI (S2035I, created by site-directed mutagenesis) DNA constructs were transiently transfected into HEK293 cells. Protein extraction and purification of Flag-mTOR and Flag-mTOR-SI were carried out 48 h later as described previously. In vitro kinase assays of purified Flag-mTOR and Flag-mTOR-SI without or with FKBP12 were done and detected by dissociation-enhanced lanthanide fluorescent immunoassay (DELFIA) as described [1].
动物实验	Mice bearing PC-3 tumors were treated with CCI-779 (1, 5, 10, and 20 mg per kg per day), or vehicle solution for 3 or 5 days per week for 3 weeks. Mice bearing DU145 tumors were only treated with CCI-779 (20 mg per kg per day) or vehicle solution for 3 weeks. Mice bearing PC-3 tumors received the following treatments: (a) control, vehicle solution for CCI-779; (b) chemotherapy alone, mitoxantrone 1.5 mg/kg or docetaxel 10 mg/kg was injected i.p. weekly for 3 doses; (c) CCI-779 alone, 5 or 10 mg/kg was injected i.p. daily, three times a week for 3 weeks; (4) chemotherapy followed by CCI-779. The largest and perpendicular diameters of tumors were measured twice weekly, and animals were coded using ear tags so that the observer was unaware of their treatment history. Tumor volume was estimated and plotted against time to evaluate response to treatment [2].
体外活性	Temsirolimus (CCI-779; 10 nmol/L至<5 μmol/L) 主要展现了一种平坦且选择性的细胞增殖抑制作用。对Temsirolimus 敏感的细胞系，其增殖被抑制≥50%，包括LNCap、PC3MM2、MDA468、H446和Caco2；而抑制率≤25%的细胞系为SW480、HT29、HCT116和H460 [1]。经过3天100 nmol/L CCI-779处理后，PC-3和DU145细胞的集落形成数分别为0.18 ± 0.09和0.37 ± 0.03 [2]。
体内活性	Temsirolimus能够以剂量依赖的方式抑制PC-3肿瘤的生长，并且对DU145肿瘤的生长抑制作用更大。经Temsirolimus（20 mg/kg i.p.）治疗5次每周，为期3周后，使肿瘤体积增长至500 mm³的平均延迟时间分别为39 ± 5天和17 ± 3天。小鼠随机接受Temsirolimus（5至10 mg/kg/d）或单纯溶媒作为对照组的治疗[2]，每周治疗6天。在所有测试样本中均观察到疾病负担的显著改善。来自3位患者（96、240和359）的异种移植小鼠在脾脏疾病体积上有统计学上显著的减少[3]。以10次腹腔注射的方式给予Temsirolimus，对8226、OPM-2和U266细胞系的皮下生长诱导了显著的剂量依赖性抗肿瘤反应。Temsirolimus的有效剂量与适度的毒性相关，仅引起短暂的血小板减少和白细胞减少。尽管在8226和OPM-2肿瘤结节中Temsirolimus对p70 mTOR底物的抑制作用相同，OPM-2肿瘤生长对于增殖、血管生成和凋亡诱导的敏感性明显更高[4]。
存储条件	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
溶解度	H2O : < 1 mg/mL (insoluble or slightly soluble) Ethanol : 70 mg/mL (67.9 mM)
关键字	Temsirolimus \| NSC-683864 \| NSC683864 \| mTOR \| Mammalian target of Rapamycin \| Inhibitor \| inhibit \| CCI779 \| CCI 779 \| Autophagy \| Apoptosis
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西罗莫司脂化物|||替西罗莫司|||NSC 683864|||CCI-779|TargetMol

上海陶术生物科技有限公司为美国Target Molecule Corp. ( Target Mol ) 在上海建立的全资子公司。我们与美国波士顿、德国慕尼黑的同事一起，为北美、欧洲和亚洲从事药物研发和生物学研究的科学家提供优质的产品和专业的服务。公司下设筛选事业部，化学事业部，生物事业部和新材料部。从虚拟筛选到实体化合物分子供应；从商业化产品销售到个性化定制合成；从对明确靶点的分子筛选到对明确分子的多靶点筛选，从高通量筛选到化学结构优化，我们都可以满足您的科研用品及技术服务的需求。经过在中国市场五年的精心耕耘，我们已成为筛选化合物领域优秀的供应商，为超过五百家学校和各类企业提供了品质卓越的小分子化合物和药物筛

成立日期	(12年)
注册资本	566.2651万人民币
员工人数	100-500人
年营业额	￥ 1亿以上
经营模式	贸易,试剂,定制,服务
主营行业	化学试剂,生物活性小分子